目的: 考察非离子表面活性剂维生素E聚乙二醇1000琥珀酸酯(TPGS)对宝藿苷I在Caco-2细胞模型转运的影响。方法: 采用Caco-2细胞模型研究不同浓度的TPGS对宝藿苷Ⅰ细胞转运行为的影响, 以超高压液相色谱(UPLC)法测定细胞样品溶液中宝藿苷I的浓度, 计算表观渗透系数(P_app)。结果: 在应用TPGS后, 宝藿苷Ⅰ从细胞绒毛面供给侧(AP)→基底面外侧(BL)的跨膜转运量明显增高(P<0.05), 外排比率显著下降(P<0.05)。当宝藿苷Ⅰ与TPGS比例分别为1∶1、1∶3、1∶9时, 宝藿苷Ⅰ的外排比率分别为1.978 8、1.779 8、1.609 0,与仅用宝藿苷Ⅰ相比分别下降了73%、76%、78%。结论: 在Caco-2细胞模型上, TPGS可显著促进宝藿苷Ⅰ的吸收。

Objective: To investigate the effect of non-ionic surfactant vitamin E tocopherol polyethylene glycol succinate 1000(TPGS) on the intestinal absorption of baohuoside I across membrane transport of Caco-2 monolayer model. Methods: The membrane transport of Caco-2 monolayer model was carried out to examine the effects of TPGS on the intestinal absorption of baohuoside I. The baohuoside I was determined by UPLC and the apparent permeability coefficients (Papp) were calculated. Results: Papp values of membrane transport capacity from the apical (AP) to basolateral (BL) of baohuoside I were significantly increased (P<0.05) and its efflux ratios were markedly reduced (P<0.05) in the presence of the TPGS. The efflux of baohuoside I was 1.9788, 1.7798, and 1.6090, respectively, when the proportion of baohuoside I and TPGS was 1:1, 1:3, and 1:9. The ratio decreased 73%, 76%, and 78% by using baohuoside I only. Conclusion: TPGS could obviously promote the absorption of baohuoside I on Caco-2 monolayer model.

国家自然科学基金资助项目(30973944)